- Discovery of pyrazolopyrimidine derivatives as novel inhibitors of ataxia telangiectasia and rad3 related protein (ATR)
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The ATR pathway is a critical mediator of the replication stress response in cells. In aberrantly proliferating cancer cells, this pathway can help maintain sufficient genomic integrity for cancer cell progression. Herein we describe the discovery of 19,
- Ramachandran, Sreekanth A.,Jadhavar, Pradeep S.,Singh, Manvendra P.,Sharma, Ankesh,Bagle, Gaurav N.,Quinn, Kevin P.,Wong, Po-yin,Protter, Andrew A.,Rai, Roopa,Pham, Son M.,Lindquist, Jeffrey N.
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Read Online
- Baker's yeast catalyzed preparation of a new enantiomerically pure synthon of (S)-pramipexole and its enantiomer (dexpramipexole) This work is dedicated to Professor Enzo Santaniello in the year of his 70th birthday
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A biocatalyzed reduction of a prochiral bicyclic ketone afforded enantiomerically pure (R)-2-acetylamino-6-hydroxy-4,5,6,7-tetrahydrobenzothiazole, a synthon of the anti-Parkinson (S)-pramipexole and its (R)-isomer, which is currently under investigation for the treatment of amyotrophic lateral sclerosis (ALS).
- Ferraboschi, Patrizia,Ciceri, Samuele,Ciuffreda, Pierangela,De Mieri, Maria,Romano, Diego,Grisenti, Paride
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p. 1239 - 1245
(2015/02/19)
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- Process for preparation of 2-amino-6 (alkyl) amino-4,5,6,7-tetrahydrobenzothiazoles
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A new process to obtain pramipexole and related products is described. The process involves the reaction of new compounds of formula (6), wherein R is hydrogen or acyl group, R3 and R4 are either the same and each of them represents an alkoxy group of 1-4 carbons or they together form a C2-C5 alkylenedioxy group or an oxo-group, with an alkylamine in the presence of a reducing agent or a hydrogen gas with hydrogenation catalyst. A process to obtain new compounds of formula (6) is also described.
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